EP0549420A1 - Forme galénique sèche et poreuse à base de plantes, son procédé de préparation et ses applications - Google Patents

Forme galénique sèche et poreuse à base de plantes, son procédé de préparation et ses applications Download PDF

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Publication number
EP0549420A1
EP0549420A1 EP92403437A EP92403437A EP0549420A1 EP 0549420 A1 EP0549420 A1 EP 0549420A1 EP 92403437 A EP92403437 A EP 92403437A EP 92403437 A EP92403437 A EP 92403437A EP 0549420 A1 EP0549420 A1 EP 0549420A1
Authority
EP
European Patent Office
Prior art keywords
plants
composition
plant
absorption promoter
dry
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP92403437A
Other languages
German (de)
English (en)
French (fr)
Inventor
Guy Derrieu
Bernard Azur Sea Raynier
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Laboratoires Ardeval
Original Assignee
Laboratoires Ardeval
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Laboratoires Ardeval filed Critical Laboratoires Ardeval
Publication of EP0549420A1 publication Critical patent/EP0549420A1/fr
Withdrawn legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/76—Salicaceae (Willow family), e.g. poplar
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/40—Cyclodextrins; Derivatives thereof

Definitions

  • the present invention relates to a solid composition based on whole plants and / or parts of fresh and / or dry plants and / or extracts, capable of being put in a dry and porous galenic form (lyophilized or equivalent), single or sprayed; such a dosage form is particularly well suited to increasing the stability and absorption of all the active ingredients of whole plants and / or parts of fresh and / or dry plants and / or extracts.
  • the invention also relates to the process for the preparation of said composition in dry form and of said porous galenic form, based on plants.
  • French Patents 2,036,890, 2,366,835 and 2,647,343 describe pharmaceutical forms having the characteristic of dissolving or disintegrating rapidly in an aqueous medium or in saliva.
  • European Patent Application 0 420 729 describes a preparation technique leading to the stabilization of whole plants and / or parts of fresh or dry plants or their extracts, which makes it possible to obtain in a stable manner in a liquid, mainly alcoholic medium, the total of the stabilized starting plant material.
  • the Applicant has found that it is possible to obtain a dry and porous galenic form from a solid composition based on plants, which is stable as well to chemical, enzymatic, bacterial or fungal degradations due to preparation and whose absorption in the mucous membranes is significantly increased.
  • the object of the present invention is therefore to provide a composition in the form solid based on whole plants and / or parts of plants, suitable for being put in a dry and porous galenical form and which better meets the needs of the practice, in particular in that it avoids all degradations of the active plant ingredients and allows absorption of all these active ingredients at the perlingual level, which furthermore prevents their degradation in the digestive tract.
  • the absorption promoter with sequestering action is chosen from cyclodextrins ⁇ , ⁇ , ⁇ or cyclodextrins polymerized or substituted, for example by methyl, ethyl, hydroxyethyl or hydroxypropyl radicals, aminocyclodextrins and maltodextrins.
  • said composition comprises as promoter absorption with sequestering action, a combination of ⁇ -cyclodextrin and maltodextrins.
  • the solid composition I has the advantage of allowing the immobilization of all the active plant ingredients present, whatever their structure and their molecular weight and allows increased stabilization of all of said active ingredients; in addition, this composition I in solid form also has the advantage of containing a minimum quantity of solvents and of being able to be put in a dry and porous galenical form, which makes it possible to further increase the absorption of said plant active ingredients, at the level of the mucous membranes.
  • the relative amount (by weight) of the active principles with respect to the absorption promoter with sequestering activity varies in proportions ranging from 5 to 50%, from preferably between 10 and 25-30% by weight.
  • said drying is carried out until complete elimination of the organic solvents and elimination of the aqueous solvents, of the order of 90%.
  • the removal of solvents can be carried out, in particular by a physical operation such as evaporation, drying, atomization, tangential filtration.
  • this is carried out under reduced pressure and is optionally associated with exposure to microwave frequencies.
  • the absorption promoter of surfactant type is chosen from glycyrrhizinic acid or one of its salts and sodium glycyrrhetinate.
  • the amount of absorption promoter of surfactant type is between 0.5 and 5% (w / w) and preferably close to 1% (w / p).
  • composition in solid form II based on plants is particularly suitable for being put in a dry and porous galenical form (lyophilized or equivalent), which exhibits an increased absorption of the plant active principles at the level of the mucous membranes.
  • the present invention also relates to a dry and porous dosage form, unitary or pulverized, characterized in that it comprises a lyophilized solid composition II, optionally combined with suitable excipients from a pharmaceutical point of view.
  • such a dry and porous galenic form based on plants has an increased absorption of the plant active ingredients because it dissolves or disintegrates quickly in an aqueous medium (saliva in particular) and facilitates the passage of all the original stabilized active ingredients. plants and / or parts of plants, through the mucous membranes (perlingual passage, for example).
  • adjuvants or absorption promoters have been mentioned in numerous publications or patents.
  • cyclodextrins they increase the absorption of cholecalciferol (DUCHENE et al., STP Pharma , 1 (1), 37-43 (1985)); vitamins A, E, K (DUCHENE D. et al., Labo Pharma Probl. , 32 (348), 842-850 (1984) and SZEJTLI J. et al., Die Paw Medicine , 32 (11), 386-391 (1980)); for sodium glycyrrhetinate, absorption insulin nasal (MISHIMA et al., J. Pharmacobio-Dyn. , 10 , s-69 (1987)); for glycyrrhizinic acid and its salts, absorption through a mucosa of calcitonin (French patent n ° 2 623 090).
  • the Applicant has surprisingly found that combining a surfactant absorption promoter, in particular glycyrrhizinic acid or one of its salts with an absorption promoter with sequestering activity ( ⁇ -cyclodextrin, for example) a synergy of the absorption of the associated active principles, at the level of the mucous membranes and more particularly at the level of the oral mucosa, which synergy of action is further increased when the said composition is porous (lyophilization).
  • a surfactant absorption promoter in particular glycyrrhizinic acid or one of its salts
  • an absorption promoter with sequestering activity ⁇ -cyclodextrin, for example
  • said dry and porous herbal dosage form also comprises suitable excipients such as diluents, binders, disintegrating or disintegrating agents and surfactants, optionally combined with optional additives such as flavorings , perfumes or sweeteners, colors, preservatives or pH correctors.
  • suitable excipients such as diluents, binders, disintegrating or disintegrating agents and surfactants, optionally combined with optional additives such as flavorings , perfumes or sweeteners, colors, preservatives or pH correctors.
  • diluents more particularly used in the dry and porous dosage forms in accordance with the invention are in particular pharmaceutical materials acceptable, preferably soluble, chosen in particular from lactose, mannitol, glycocolle, sorbitol, or mixtures of these substances.
  • the binders more particularly used in the galenical forms in accordance with the invention are in particular any material soluble or dispersible in water, capable of ensuring the cohesion of said compositions, and inert with respect to the active principles.
  • These materials are preferably chosen from polysaccharides, such as for example natural gums of the gum arabic type, alginates, pectins, gelatin, synthetic gums of the xanthan gum type, dextrans, dextrin, cellulose derivatives, polyvinyl alcohol, polyvinylpyrrolidone, or mixtures of these substances.
  • the disintegrating or disintegrating agents, the surfactants, the flavors, the perfumes or sweeteners, the colorings, the preservatives, the pH correctors are those usually used in the pharmaceutical and food industry for the development of comparable and compatible forms. with the active ingredients present.
  • said elimination comprises the complete elimination of organic solvents and the elimination of aqueous solvents, of the order of 90%.
  • the elimination of the solvents is preceded by a concentration, for example by osmosis.
  • the plant active ingredients obtained in an alcoholic medium according to European Patent Application 0 420 729 are immobilized by addition of the absorption promoter (s) with sequestering activity (coprecipitation).
  • the relative amount (by weight) of the active principles with respect to the absorption promoters with sequestering activity varies in proportions ranging from 5 to 50%, preferably between 10 and 25- 30% by weight.
  • the amount of absorption promoter of surfactant type is between 0.5 and 5% (w / w) and preferably close to 1% (w / w).
  • dry and porous dosage forms in accordance with the invention find application in the pharmaceutical, veterinary, dietetic, food or cosmetic fields.
  • the invention also comprises other provisions, which will emerge from the description which follows, which refers to examples of compositions and implementation of the method, objects of the present invention.
  • a preparation made as described above in example 3 is compared, containing ⁇ -cyclodextrin and ammonium glycyrrhizinate as absorption promoters, respectively with sequestering activity and of surfactant type, in an absorption test by the mucous membranes.
  • TEST 1 object of the invention
  • TEST 2 TEST 3
  • TEST 4 Nettle root solution (with reference to ⁇ -sitosterol) 5.2 mg 5.2 mg 5.2 mg 5.2 mg ⁇ -cyclodextrin 285 mg 285 mg - -
  • the absorption is determined by the oral absorption test described by BECKETT AH and TRIGGS EJ, J. Pharm. Pharmacol., 19 , 318-418, 1967. Two volunteers are given two oral lyophilisates, the equivalent of 10.4 mg of ⁇ -sitosterol. The level of ⁇ -sitosterol absorbed by the mucous membranes is determined by CPG assay.
  • Test 1 which corresponds to the administration of a composition in accordance with the invention, presents a absorption significantly improved compared to other tests.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Medicinal Preparation (AREA)
EP92403437A 1991-12-23 1992-12-17 Forme galénique sèche et poreuse à base de plantes, son procédé de préparation et ses applications Withdrawn EP0549420A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9115983 1991-12-23
FR9115983A FR2685205A1 (fr) 1991-12-23 1991-12-23 Composition a base de plantes sous forme solide, son procede de preparation et ses applications.

Publications (1)

Publication Number Publication Date
EP0549420A1 true EP0549420A1 (fr) 1993-06-30

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Family Applications (1)

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EP92403437A Withdrawn EP0549420A1 (fr) 1991-12-23 1992-12-17 Forme galénique sèche et poreuse à base de plantes, son procédé de préparation et ses applications

Country Status (3)

Country Link
US (1) US5527783A (enrdf_load_stackoverflow)
EP (1) EP0549420A1 (enrdf_load_stackoverflow)
FR (1) FR2685205A1 (enrdf_load_stackoverflow)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5527783A (en) * 1991-12-23 1996-06-18 Laboratoires Ardeval Dry and Porous galenic form based on plants, its method of preparation and its applications
WO2000057856A1 (fr) * 1999-03-31 2000-10-05 Pierre Fabre Medicament Composition ou structure microporeuse expansee isotrope a dissolution rapide a usage pharmaceutique, veterinaire, dietetique, alimentaire ou cosmetique et son procede d'obtention

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5549906A (en) 1993-07-26 1996-08-27 Pharmacia Ab Nicotine lozenge and therapeutic method for smoking cessation
US20060073188A1 (en) * 1999-03-31 2006-04-06 Pierre Fabre Medicament Fast-dissolving isotropic expanded microporous composition or structure for pharmaceutical, veterinary, dietetic, food or cosmetic use and method for obtaining same
US7939479B2 (en) * 2008-03-12 2011-05-10 Chandler Barry E Dry hand cleaner comprising corncob particles
MX2013007379A (es) 2010-12-21 2013-07-15 Bayer Cropscience Lp Mutantes tipo papel lija de bacillus y metodos de uso de los mismos para mejorar el crecimiento vegetal, promover la salud de plantas y controlar enfermedades y plagas.
BR112014005654A2 (pt) 2011-09-12 2017-03-28 Bayer Cropscience Lp métodos para melhorar a saúde e promover o crescimento de uma planta e/ou de melhorar o amadurecimento da fruta
US9428425B2 (en) 2012-09-20 2016-08-30 Core Intellectual Properties Holdings, Llc Methods and compositions for treating soil and plants

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0397447A1 (en) * 1989-05-12 1990-11-14 Smithkline Beecham Farmaceutici S.p.A. Pharmaceutical compositions
EP0420729A1 (fr) * 1989-09-28 1991-04-03 Laboratoires Ardeval Procédé de préparation de suspensions homogènes de plantes et suspensions homogènes ainsi obtenues

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL65184A0 (en) * 1982-03-05 1982-05-31 Yissum Res Dev Co Preparation for the treatment of oral diseases,comprising glycyrrhizin
FR2685205A1 (fr) * 1991-12-23 1993-06-25 Ardeval Laboratoires Composition a base de plantes sous forme solide, son procede de preparation et ses applications.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0397447A1 (en) * 1989-05-12 1990-11-14 Smithkline Beecham Farmaceutici S.p.A. Pharmaceutical compositions
EP0420729A1 (fr) * 1989-09-28 1991-04-03 Laboratoires Ardeval Procédé de préparation de suspensions homogènes de plantes et suspensions homogènes ainsi obtenues

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5527783A (en) * 1991-12-23 1996-06-18 Laboratoires Ardeval Dry and Porous galenic form based on plants, its method of preparation and its applications
WO2000057856A1 (fr) * 1999-03-31 2000-10-05 Pierre Fabre Medicament Composition ou structure microporeuse expansee isotrope a dissolution rapide a usage pharmaceutique, veterinaire, dietetique, alimentaire ou cosmetique et son procede d'obtention
FR2791569A1 (fr) * 1999-03-31 2000-10-06 Pf Medicament Composition ou structure microporeuse expansee isotrope a dissolution rapide a usage pharmaceutique, veterinaire, dietetique, alimentaire ou cosmetique et son procede d'obtention

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Publication number Publication date
US5527783A (en) 1996-06-18
FR2685205B1 (enrdf_load_stackoverflow) 1995-05-12
FR2685205A1 (fr) 1993-06-25

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